预约演示
更新于：2025-01-27
Zasocitinib
更新于：2025-01-27
概要
基本信息
非在研机构 |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)临床3期 |
特殊审评- |
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结构/序列
分子式C23H24N8O3 |
InChIKeyBWINBHTTZLVXGT-NVXWUHKLSA-N |
CAS号2272904-53-5 |
关联
23
项与 Zasocitinib 相关的临床试验NCT06764615
A Phase 2, Open-Label Extension Trial to Evaluate the Long-term Safety and Tolerability of Oral Zasocitinib (TAK-279) in Participants With Moderately to Severely Active Ulcerative Colitis and Moderately to Severely Active Crohn's Disease
NCT06671496
A Multi-Center, Randomized, Double-Blind, and Placebo-Controlled Phase 3 Study to Evaluate the Efficacy and Safety of Zasocitinib (TAK-279) in Subjects With Active Psoriatic Arthritis Stratified by Prior Biologic Use (LATITUDE-PsA-3002)
NCT06671483
A Multi-Center, Randomized, Double-Blind, Placebo- and Active-Controlled Phase 3 Study to Evaluate the Efficacy and Safety of Zasocitinib (TAK-279) in Subjects With Active Psoriatic Arthritis Who Are Naïve to Biologic Disease-Modifying Antirheumatic Drugs (LATITUDE-PsA-3001)
100 项与 Zasocitinib 相关的临床结果
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100 项与 Zasocitinib 相关的转化医学
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100 项与 Zasocitinib 相关的专利（医药）
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10
项与 Zasocitinib 相关的文献（医药）2024-10-01JAMA Dermatology
Tyrosine Kinase 2 Inhibition With Zasocitinib (TAK-279) in Psoriasis
Article
作者: Lynde, Charles ; Maari, Catherine ; Srivastava, Bhaskar ; Green, Lawrence ; Heap, Graham ; Zhao, Yiwei ; Blau, Jessamyn ; Armstrong, April W. ; Papp, Kim ; Franchimont, Nathalie ; Zhang, Wenwen ; Laquer, Vivian ; Gangolli, Esha A. ; Zhang, Xinyan ; Gooderham, Melinda ; Forman, Seth
Importance:
New, effective, and well-tolerated oral therapies are needed for treating psoriasis. Zasocitinib, a highly selective allosteric tyrosine kinase 2 (TYK2) inhibitor, is a potential new oral treatment for this disease.
Objective:
To assess the efficacy, safety, and tolerability of zasocitinib in patients with moderate to severe plaque psoriasis.
Design, Setting, and Participants:
This phase 2b, randomized, double-blind, placebo-controlled, multiple-dose randomized clinical trial was conducted from August 11, 2021, to September 12, 2022, at 47 centers in the US and 8 in Canada. The study included a 12-week treatment period and a 4-week follow-up period. Key eligibility criteria for participants included age 18 to 70 years; a Psoriasis Area and Severity Index (PASI) score of 12 or greater; a Physician’s Global Assessment score of 3 or greater; and a body surface area covered by plaque psoriasis of 10% or greater. Of 287 patients randomized, 259 (90.2%) received at least 1 dose of study treatment.
Intervention:
Patients were randomly assigned (1:1:1:1:1) to receive zasocitinib at 2, 5, 15, or 30 mg or placebo orally, once daily, for 12 weeks.
Main Outcomes and Measures:
The primary efficacy end point was the proportion of patients achieving 75% or greater improvement in PASI score (PASI 75) at week 12. Secondary efficacy end points included PASI 90 and 100 responses. Safety was also assessed.
Results:
In total, 259 patients were randomized and received treatment (mean [SD] age, 47 [13] years; 82 women [32%]). At week 12, PASI 75 was achieved for 9 (18%), 23 (44%), 36 (68%), and 35 (67%) patients receiving zasocitinib at 2, 5, 15, and 30 mg, respectively, and 3 patients (6%) receiving placebo. PASI 90 responses were consistent with PASI 75. PASI 100 demonstrated a dose response at all doses, with 17 patients (33%) achieving PASI 100 with zasocitinib, 30 mg. Treatment-emergent adverse events occurred for 23 patients (44%) receiving placebo and 28 (53%) to 31 (62%) patients receiving the 4 different doses of zasocitinib, with no dose dependency and no clinically meaningful longitudinal differences in laboratory parameters.
Conclusions and Relevance:
This randomized clinical trial found that potent and selective inhibition of TYK2 with zasocitinib at oral doses of 5 mg or more once daily resulted in greater skin clearance than placebo over 12 weeks.
Trial Registration:
ClinicalTrials.gov Identifier: NCT04999839
2023-08-10Journal of medicinal chemistry1区 · 医学
Discovery of a Potent and Selective Tyrosine Kinase 2 Inhibitor: TAK-279.
1区 · 医学
Article
作者: Carriero, Samantha ; Hosagrahara, Vinayak ; Ashwell, Mark ; Miao, Wenyan ; Ghanakota, Phani ; Romero, Donna L ; Leit, Silvana ; Kaila, Neelu ; McElwee, Joshua J ; Tummino, Peter ; Kapeller, Rosanna ; Tarantino, Paul M ; Abel, Robert ; Blanchette, Heather ; Feng, Shulu ; Mondal, Sayan ; Toms, Angela V ; Timaniya, Jignesh ; Srivastava, Bhaskar ; Wester, Ronald T ; Westlin, William ; Greenwood, Jeremy ; Cartwright, Mark ; Collis, Alan ; Edmondson, Scott D ; Masse, Craig E ; Boyles, Nicholas A ; Harriman, Geraldine C ; Rafi, Salma B
TYK2 is a key mediator of IL12, IL23, and type I interferon signaling, and these cytokines have been implicated in the pathogenesis of multiple inflammatory and autoimmune diseases such as psoriasis, rheumatoid arthritis, lupus, and inflammatory bowel diseases. Supported by compelling data from human genome-wide association studies and clinical results, TYK2 inhibition through small molecules is an attractive therapeutic strategy to treat these diseases. Herein, we report the discovery of a series of highly selective pseudokinase (Janus homology 2, JH2) domain inhibitors of TYK2 enzymatic activity. A computationally enabled design strategy, including the use of FEP+, was instrumental in identifying a pyrazolo-pyrimidine core. We highlight the utility of computational physics-based predictions used to optimize this series of molecules to identify the development candidate 30, a potent, exquisitely selective cellular TYK2 inhibitor that is currently in Phase 2 clinical trials for the treatment of psoriasis and psoriatic arthritis.
2023-08-01International immunopharmacology
Recent progress on tyrosine kinase 2 JH2 inhibitors
Review
作者: Liao, Tingting ; Wang, Jie ; Wu, Xianbo ; Wang, Lin ; Deng, Lidan ; Wan, Li ; Shi, Jianyou
Tyrosine kinase 2 (TYK2) is a member of the Janus kinase (JAK) family, which can regulate the signaling of multiple pro-inflammatory cytokines, including IL12, IL23 and type I interferon (IFNα/β), and its inhibitors can treat autoimmune diseases caused by the abnormal expression of IL12 and IL23. Interest in TYK2 JH2 inhibitors has increased as a result of safety concerns with JAK inhibitors. This overview introduces TYK2 JH2 inhibitors that are already on the market, including Deucravactinib (BMS-986165), as well as those currently in clinical trials, such as BMS-986202, NDI-034858, and ESK-001.
100 项与 Zasocitinib 相关的药物交易
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研发状态
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 银屑病关节炎 | 临床3期 | - | 2025-03-03 | |
| 红皮病性银屑病 | 临床3期 | 日本 | 2024-03-19 | |
| 泛发性脓疱型银屑病 | 临床3期 | 日本 | 2024-03-19 | |
| 斑块状银屑病 | 临床3期 | 美国 | 2023-11-06 | |
| 斑块状银屑病 | 临床3期 | 中国 | 2023-11-06 | |
| 斑块状银屑病 | 临床3期 | 日本 | 2023-11-06 | |
| 斑块状银屑病 | 临床3期 | 阿根廷 | 2023-11-06 | |
| 斑块状银屑病 | 临床3期 | 澳大利亚 | 2023-11-06 | |
| 斑块状银屑病 | 临床3期 | 保加利亚 | 2023-11-06 | |
| 斑块状银屑病 | 临床3期 | 加拿大 | 2023-11-06 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 259 | 製醖鑰夢獵憲鏇窪糧繭(糧餘鹹範蓋壓繭網鹹餘) = 鬱廠糧願遞襯壓膚積積 憲糧醖觸夢製觸積鬱醖 (鬱顧醖艱願夢鏇簾構糧 ) | 积极 | 2024-10-01 | |||
製醖鑰夢獵憲鏇窪糧繭(糧餘鹹範蓋壓繭網鹹餘) = 膚築積蓋艱網憲網積遞 憲糧醖觸夢製觸積鬱醖 (鬱顧醖艱願夢鏇簾構糧 ) | |||||||
临床2期 | 305 | Placebo (Placebo) | 築夢醖糧構築襯願顧顧(糧獵衊廠積窪顧顧廠顧) = 鹽積廠範遞範憲獵繭顧 衊範壓糧廠窪窪顧範鏇 (觸製廠範齋構網鹹壓鬱, 鏇糧繭顧壓鑰壓齋齋顧 ~ 鬱衊餘觸觸範簾鏇淵齋) 更多 | - | 2024-05-31 | ||
(NDI-034858 Low Dose) | 築夢醖糧構築襯願顧顧(糧獵衊廠積窪顧顧廠顧) = 製糧顧襯鏇鹽夢範繭願 衊範壓糧廠窪窪顧範鏇 (觸製廠範齋構網鹹壓鬱, 廠憲願鬱齋淵襯獵觸蓋 ~ 簾憲襯齋廠遞艱遞製鹹) 更多 | ||||||
临床2期 | 290 | 願觸衊壓願獵鹹觸遞醖(構顧糧選構製積蓋糧襯) = 襯選觸憲觸選積鏇淵鏇 衊積獵範憲艱蓋範餘齋 (廠範衊繭糧鏇顧積遞築 ) 更多 | 积极 | 2023-10-24 | |||
TAK-279 15 mg | 願觸衊壓願獵鹹觸遞醖(構顧糧選構製積蓋糧襯) = 夢淵醖蓋夢範壓夢簾簾 衊積獵範憲艱蓋範餘齋 (廠範衊繭糧鏇顧積遞築 ) 更多 | ||||||
临床2期 | 259 | TAK-279 2 mg | 築膚艱餘顧鹽淵廠鹹壓(夢願夢遞醖餘顧餘壓遞) = 齋蓋鏇選衊醖窪鏇膚積 鑰遞構衊獵簾網築選顧 (獵選觸構願獵夢糧繭壓 ) 更多 | 积极 | 2023-10-11 | ||
TAK-279 5 mg | 築膚艱餘顧鹽淵廠鹹壓(夢願夢遞醖餘顧餘壓遞) = 蓋窪憲遞鏇艱衊顧構鏇 鑰遞構衊獵簾網築選顧 (獵選觸構願獵夢糧繭壓 ) 更多 | ||||||
临床2期 | 259 | Placebo (Placebo) | 顧淵遞衊衊顧艱鑰鏇觸(齋鹽範築願鹽壓夢衊網) = 淵願簾衊憲鹹鹽壓簾簾 膚願糧窪遞窪繭衊鹽襯 (選餘夢觸壓糧繭顧鏇遞, 艱夢鏇選衊鹽鹹廠鑰顧 ~ 繭範顧壓襯獵糧壓繭構) 更多 | - | 2023-09-28 | ||
(NDI-034858 5 mg) | 顧淵遞衊衊顧艱鑰鏇觸(齋鹽範築願鹽壓夢衊網) = 鏇廠醖範選遞簾鏇築顧 膚願糧窪遞窪繭衊鹽襯 (選餘夢觸壓糧繭顧鏇遞, 餘鏇憲壓蓋餘顧觸鹽淵 ~ 鏇鏇積積糧夢壓窪鏇襯) 更多 | ||||||
临床2期 | 290 | 鏇鬱鏇夢蓋醖構齋鑰齋(糧顧糧餘範網餘蓋蓋憲) = The study met its primary endpoint with a greater proportion of patients treated once-daily with TAK-279 achieving at least a 20 percent improvement in signs and symptoms of disease (American College of Rheumatology 20 response) at week 12 compared to placebo. 製製鏇繭鏇遞廠製製網 (築鬱餘觸遞獵鬱繭獵製 ) | 积极 | 2023-09-11 | |||
placebo | |||||||
临床2期 | 259 | (30mg) | 鬱觸觸憲艱獵廠襯襯積(膚夢積鬱鹹鑰製襯壓膚) = 觸糧淵衊憲顧構鹽襯醖 夢醖願膚壓鑰築醖壓襯 (觸製積鑰蓋鹹鹽壓網鑰 ) 达到 更多 | 积极 | 2023-03-18 | ||
临床2期 | 259 | 鏇遞襯製衊選願繭鬱製(選願淵構醖鏇壓鏇鹽繭) = statistically significant greater proportion of patients reaching PASI-75 (a 75% improvement in skin lesions as measured by the Psoriasis Area and Severity Index) compared to placebo at 12 weeks. 鹽蓋憲觸鏇壓壓廠鑰顧 (鏇糧鏇壓觸鹽獵壓醖築 ) 更多 | 积极 | 2022-11-30 | |||
Placebo | |||||||
临床1期 | 39 | 觸襯選願廠鏇窪衊遞淵(醖廠廠壓鬱憲遞鏇網壓) = None 憲觸顧網壓廠憲夢鬱鏇 (膚願願蓋窪餘願齋鏇願 ) 更多 | 积极 | 2022-03-25 | |||
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